Patents Examined by Samantha L Shterengarts
  • Patent number: 10851081
    Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: April 29, 2020
    Date of Patent: December 1, 2020
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Scott W. Bagley, John M. Curto, Matthew S. Dowling, David Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Gajendra Ingle, Wenhua Jiao, Chris Limberakis, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
  • Patent number: 10851110
    Abstract: The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.
    Type: Grant
    Filed: February 7, 2019
    Date of Patent: December 1, 2020
    Inventors: Philip Jones, Barbara Czako, Jason Cross, Paul Leonard, Faika Mseeh, Connor Austin Parker
  • Patent number: 10842793
    Abstract: The present invention relates to compounds that have the capability of inhibiting the secretion of fibroblast growth factor 2 (FGF2) by tumor cells, as well as uses of said compound in medicine, in particular in the prevention and/or treatment of cancerous or inflammatory diseases.
    Type: Grant
    Filed: February 7, 2017
    Date of Patent: November 24, 2020
    Assignees: Universitat Heidelberg, European Molecular Biology Laboratory
    Inventors: Walter Nickel, Joe Lewis
  • Patent number: 10844074
    Abstract: Compounds having the general formula (I) and pharmaceutical compositions that can be used as Bruton's Tyrosine Kinase (BTK), ITK, JAK3, and selective mutant epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor and their uses in the treatment of related diseases and disorders such as cancer.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: November 24, 2020
    Inventors: Haixiao Zhai, Fan Wu, Zhanggui Wu
  • Patent number: 10836707
    Abstract: Disclosed are a mild and efficient preparation method for an ?-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The ?-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced ?-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.
    Type: Grant
    Filed: January 20, 2017
    Date of Patent: November 17, 2020
    Inventors: Junfeng Zhao, Long Hu, Silin Xu, Zhenguang Zhao
  • Patent number: 10835616
    Abstract: The invention relates to novel conjugating reagents capable of reaction with at least one nucleophile present in a peptide or protein, which contain at least one leaving group which is lost on reaction with said nucleophile, in which the leaving group includes a portion —(CH2CH2O)n—, in which n is a number of six or more; and novel processes for the preparation of conjugates containing peptides or proteins made using such reagents.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: November 17, 2020
    Inventors: Antony Godwin, George Badescu, Matthew Bird, Penny Bryant, David Morris, Mark Frigerio
  • Patent number: 10821107
    Abstract: The subject invention concerns materials and methods for treating depression, stress disorders, such as PTSD, anxiety disorders, and/or a neurodegenerative disease or condition in a person or animal. In one embodiment, a person or animal in need of treatment is administered one or more compounds or drugs, or a composition comprising the one or more compounds or drugs, that inhibit FKBP51 activity or function. The subject invention also concerns a method for inhibiting activity of the FKBP51 protein in a cell. The subject invention also concerns methods of screening for compounds or drugs that inhibit the FKBP51 protein.
    Type: Grant
    Filed: April 10, 2018
    Date of Patent: November 3, 2020
    Inventors: Jonathan Jacob Sabbagh, Chad Dickey
  • Patent number: 10815184
    Abstract: The present disclosure provides co-crystals of a lithium benzoate compound and a co-former compound of Formula (I) Also provided herein are methods of preparing the co-crystals and uses thereof in treating and/or reducing the risk for a neuropsychiatric disorder (e.g., schizophrenia, psychotic disorders, depressive disorders, bipolar disorders, or neurodegenerative disorders).
    Type: Grant
    Filed: June 13, 2017
    Date of Patent: October 27, 2020
    Assignee: SyneuRX International (Taiwan) Corp.
    Inventors: Guochuan Emil Tsai, Ching-Cheng Wang, Tien-Lan Hsieh, Yuan-Chun Lo
  • Patent number: 10800768
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
    Type: Grant
    Filed: April 2, 2019
    Date of Patent: October 13, 2020
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Jingwei Li, Wenqing Yao, Chao Qi, Ding-Quan Qian, Fenglei Zhang
  • Patent number: 10800743
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: October 13, 2020
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
  • Patent number: 10793582
    Abstract: Provided are a novel compound having a superior inhibitory action on KAT-II, a production method thereof, use thereof, and a pharmaceutical composition containing the aforementioned compound and the like. A compound represented by the formula (I) or a pharmacologically acceptable salt thereof. wherein each symbol is as defined in the DESCRIPTION.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: October 6, 2020
    Inventors: Masahiro Okuyama, Kenji Fukunaga, Kenji Usui, Norimitsu Hayashi, Daisuke Iijima, Hideki Horiuchi, Nobuaki Fujimoto
  • Patent number: 10793525
    Abstract: The synthesis and in vitro and in vivo anti-breast and anti-prostate cancers activities of novel C-4 heteroaryl 13-cis retinamides that modulate Mnk-eIF4E and AR signaling are discussed. In both breast and prostate cancer cell lines, these compounds induce Mnk1/2 degradation to substantially suppress eIF4E phosphorylation. In prostate cancer cells, the compounds induce degradation of both full-length androgen receptor (fAR) and splice variant AR (AR-V7) to inhibit AR transcriptional activity. The consequences of these multiple activities resulted in inhibition of cell growth and migration and induction of apoptosis. Finally and importantly, the compounds demonstrate strong in vitro and in vivo anti-breast and anti-prostate cancer activities, with no apparent host toxicities.
    Type: Grant
    Filed: November 18, 2015
    Date of Patent: October 6, 2020
    Inventors: Vincent Njar, Hannah Mbatia, Vidya Ramamurthy, Senthilmurugan Ramalingam
  • Patent number: 10793578
    Abstract: A series of fused pentacyclic imidazole derivatives, being potent modulators of f benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 5,7,8,15-tetrahydro-6H-8,15-methanobenzimidazo[1,2-b][2,5]benzodiazocin-6-one derivatives and analogs thereof.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: October 6, 2020
    Assignees: UCB Biopharma SRL, Sanofi
    Inventors: Jag Paul Heer, Jean Keyaerts
  • Patent number: 10787435
    Abstract: The present disclosure relates to a compound as shown in formula (II), a tautomer or a pharmaceutically acceptable salt thereof, and disclosed is the use thereof in preparing a drug for treating an ASK1-associated disease.
    Type: Grant
    Filed: January 22, 2018
    Date of Patent: September 29, 2020
    Assignee: Fuijan Cosunter Pharmaceutical Co. Ltd.
    Inventors: Chengde Wu, Tao Yu, Ning Li, Shuhui Chen
  • Patent number: 10786520
    Abstract: Novel pseudo-trisaccharide aminoglycosides, represented by Formula I, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: September 29, 2020
    Inventor: Timor Baasov
  • Patent number: 10774169
    Abstract: The present application relates to brush amphiphilic block copolymers comprising at least one block which is hydrophilic and at least another block which is hydrophobic.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: September 15, 2020
    Assignee: McMaster University
    Inventors: Lukas Sadowski, Todd Hoare, Haiming (Daniel) Luo, Maryam Badv
  • Patent number: 10774053
    Abstract: The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: September 15, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Zhenhong R. Cai, Aesop Cho, Ana Zurisadai Gonzalez Buenrostro, Xiaochun Han, Salman Y. Jabri, Ryan McFadden, Yingmei Qi, Johannes Voigt, Hong Yang, Jie Xu, Lianhong Xu
  • Patent number: 10765645
    Abstract: This application describes a compound represented by Formula (I): YZX1—S(O)(X2)F)m]n??(I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: September 8, 2020
    Inventors: Jiajia Dong, K. Barry Sharpless, Jeffery W. Kelly, Aleksandra Baranczak, Wentao Chen
  • Patent number: 10766863
    Abstract: The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and/or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.
    Type: Grant
    Filed: November 17, 2015
    Date of Patent: September 8, 2020
    Inventors: Vincent Sandanayaka, Qiong Wu
  • Patent number: 10759752
    Abstract: The present invention relates to a composition for the modulation of the activity of non-structure proteins and a compound contained therein.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: September 1, 2020
    Assignee: Eberhard Karls Universitaet Tuebingen Medizinische Fakultaet
    Inventors: Bernhard Hirt, Claus Zeyher, Corinna Gleiser, Lothar Just